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Thiopurines: Factors influencing toxicity and response
Karolinska Institute.
Linköping University, Department of Medicine and Health Sciences, Pharmacology . Linköping University, Faculty of Health Sciences. (Newcastle University)
Karolinska Institute.
2010 (English)In: BIOCHEMICAL PHARMACOLOGY, ISSN 0006-2952, Vol. 79, no 9, 1211-1220 p.Article in journal (Refereed) Published
Abstract [en]

Thiopurines are the backbone of current anti-leukemia regimens and have also been effective immunosuppressive agents for the past half a century. Extensive research on their mechanism of action has been undertaken, yet many issues remain to be addressed to resolve unexplained cases of thiopurine toxicity or treatment failure. The aim of this review is to summarize current knowledge of the mechanism of thiopurine action in experimental models and put into context with clinical observations. Clear understanding of their metabolism will contribute to maximizing efficacy and minimizing toxicity by individually tailoring therapy according to the expression profile of relevant factors involved in thiopurine activation pathway.

Place, publisher, year, edition, pages
2010. Vol. 79, no 9, 1211-1220 p.
Keyword [en]
Acute lymphoblastic leukemia, 6-Mercaptopurine, 6-Thioguanine, Azathioprine, Hypoxanthine-guanine phosphoribosyl transferase, Thiopurine methyltransferase, Inosine 5 -monophosphate dehydrogenase, Transport, Pharmacogenetics
National Category
Medical and Health Sciences
URN: urn:nbn:se:liu:diva-54718DOI: 10.1016/j.bcp.2010.01.006ISI: 000275681900001OAI: diva2:308394
Available from: 2010-04-06 Created: 2010-04-06 Last updated: 2010-04-06

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